Potent and selective adenosine A2A receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones

被引：19

作者：

Harris, Joel M. ^{[1
]}

Neustadt, Bernard R. ^{[1
]}

Zhang, Hongtao ^{[1
]}

Lachowicz, Jean ^{[1
]}

Cohen-Williams, Mary ^{[1
]}

Varty, Geoff ^{[1
]}

Hao, Jinsong ^{[1
]}

Stamford, Andrew W. ^{[1
]}

机构：

[1] Merck Res Labs, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 08期

关键词：

Adenosine; A(2A); A(2A) receptor; A(2A) antagonist; Adenosine receptor; Parkinson's disease; PARKINSONS-DISEASE; DISCOVERY; ISTRADEFYLLINE; DERIVATIVES;

D O I：

10.1016/j.bmcl.2011.02.045

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Antagonism of the adenosine A(2A) receptor affords a possible treatment of Parkinson's disease. In the course of investigating pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A(2A) antagonists, we prepared [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones with potent and selective (vs A(1)) A(2A) antagonist activity. Structure-activity relationships are described for this series. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：2497 / 2501

页数：5

共 34 条

[21] The discovery and synthesis of novel adenosine receptor (A2A) antagonists [J].

Matasi, JJ ;

Caldwell, JP ;

Hao, JS ;

Neustadt, B ;

Arik, L ;

Foster, CJ ;

Lachowicz, J ;

Tulshian, DB .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (05) :1333-1336

[22] 2,6-diaryl-4-acylaminopyrimidines as potent and selective adenosine A2A antagonists with improved solubility and metabolic stability [J].

Moorjani, Manisha ;

Luo, Zhiyong ;

Lin, Emily ;

Vong, Binh G. ;

Chen, Yongsheng ;

Zhang, Xiaohu ;

Rueter, Jaimie K. ;

Gross, Raymond S. ;

Lanier, Marion C. ;

Tellew, John E. ;

Williams, John P. ;

Lechner, Sandra M. ;

Malany, Siobhan ;

Santos, Mark ;

Crespo, Maria I. ;

Diaz, Jose-Luis ;

Saunders, John ;

Slee, Deborah H. .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (20) :5402-5405

[23] A2A adenosine receptor antagonists -: future drugs for Parkinson's disease? [J].

Müller, CE .

DRUGS OF THE FUTURE, 2000, 25 (10) :1043-1052

[24]

Neustadt B. R., 2005, Preparation of pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2A receptor antagonists, Patent No. [US-20050239795, 20050239795]

[25] Potent, selective, and orally active adenosine A2A receptor antagonists:: Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines [J].